IP Library › Granted Patent US 8,778,950
Granted Patent B2
US 8,778,950 · App. 13/392,074 · Granted Jul 15, 2014

Cannabinoid receptor modulators

Inventors: Robert M. Jones (San Diego, CA); Sangdon Han (San Diego, CA); Lars Thoresen (San Diego, CA); Jae-Kyu Jung (San Diego, CA); Sonja Strah-Pleynet (Newton, MA); Xiuwen Zhu (San Diego, CA); Yifeng Xiong (San Diego, CA); Dawei Yue (San Diego, CA)
Assignee: Arena Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,778,950
App. No.
13/392,074
Granted
Jul 15, 2014
Kind
B2
Abstract

The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

Claims (8)

1. A compound selected from the following compound and pharmaceutically acceptable salts, solvates, and hydrates thereof:

(1aS,5aS)-2-Pyrazin-2-yl-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 696).

2. A compound selected from the following compound and pharmaceutically acceptable salts, solvates, and hydrates thereof:

(1aS,5aS)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 699).

3. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

4. A pharmaceutical composition comprising a compound according to claim 2 and a pharmaceutically acceptable carrier.

5. A process for preparing a pharmaceutical composition comprising admixing a compound according to claim 1 and a pharmaceutically acceptable carrier.

6. A process for preparing a pharmaceutical composition comprising admixing a compound according to claim 2 and a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 8, 2012
From: JONES, ROBERT M.; HAN, SANGDON; THORESEN, LARS; JUNG, JAE-KYU; STRAH-PLEYNET, SONJA; ZHU, XIUWEN; XIONG, YIFENG; YUE, DAWEI
To: ARENA PHARMACEUTICALS, INC.
Reel/Frame 028177/0848 →
Continuity (1)
Related Publication 20120214766A1 · Aug 23, 2012